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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Research Article

Design, Synthesis and In-vivo Anti-inflammatory Activity of New Celecoxib Analogues as NSAID

Author(s): Naglaa A. Abdel Hafez, Korany A. Ali*, Alhussein A. Ibrahim, Dina H. Elnaggar and Amany A. Sleem

Volume 18, Issue 16, 2018

Page: [1398 - 1408] Pages: 11

DOI: 10.2174/1389557518666180530124509

Price: $65


Background: A new series of Celecoxib analogues were easily synthesized via reactions of 4-(2-(1-chloro-2-oxopropylidene)hydrazinyl)benzene sulfonamide (1) with active methylene compounds and dialkyl malonate. In addition, compound 1 was reacted also with thiourea derivatives and thiosemicarbazone derivatives to afford thiazole derivatives 9 and 11, respectively. Furthermore, triazolo pyrimidine derivatives 13 were prepared via reaction of compound 1 with pyrimidine thione derivatives. The structures of the new synthesized compounds were assigned by elemental analysis and spectroscopic data. The new analogues were screened for their in vivo anti-inflammatory activity using carrageenan-induced paw edema method.

Conclusion: They showed moderate to good in vivo anti-inflammatory effects. Compounds 1, 6 and 11b were the most active compounds that reduced the paw edema induced by carrageenan by 12.25 %, 12.96 % and 12.97% respectively, as compared to the Indomethacin that inhibited the oedema volume by 7.47 %.

Keywords: Anti-inflammatory Activity, Hydrazonoyl halide, pyrazole, thiazole, sulphonamide, NSAID` drugs.

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